Related Experiment Videos
In vitro evaluation of gentamicin released from microparticles
M J Blanco-Príeto1, C Lecaroz, M J Renedo
1Department of Pharmacy and Pharmaceutical Technology, University of Navarra, 31080, Pamplona, Spain. mjblanco@unav.es
Abstract:
In this study, the preparation, characterization and drug release behaviour of gentamicin (GM)-loaded poly(D,L-lactide-co-glycolide) microspheres are described. The microspheres were produced using a double emulsion solvent evaporation technique. All the microspheres preparation resulted in spherical shape and the mean diameter was 3 microm (for empty microspheres) and between 5 and 9 microm for microparticles loaded with GM. The encapsulation efficiency (EE) ranged from 3.4 to 90% depending on the formulation. Increasing the volume of the external aqueous phase, increased the EE. Encapsulation also depended on the pH value of the internal aqueous phase, the highest value was achieved when maintained the internal aqueous phase at pH 6, where GM was more soluble. Moreover, increasing nominal GM loading yielded lower encapsulation efficiencies. The release profiles of GM from microparticles resulted in biphasic patterns. After an initial burst, a continuous drug release was observed for up to 4 weeks. Finally, the formulations with higher loading released the drug faster.
Insights
This study details gentamicin (GM)-loaded poly(D,L-lactide-co-glycolide) microspheres, optimizing encapsulation efficiency and characterizing drug release. Formulations with higher loading released GM faster, showing biphasic release patterns over 4 weeks.
Area of Science:
- Biomaterials Science
- Drug Delivery Systems
- Polymer Chemistry
Background:
- Poly(D,L-lactide-co-glycolide) (PLGA) microspheres are widely used for controlled drug delivery.
- Gentamicin (GM) is a crucial antibiotic for treating bacterial infections, often requiring sustained release formulations.
- Optimizing the preparation and characterization of GM-loaded PLGA microspheres is essential for effective therapeutic outcomes.
Purpose of the Study:
- To prepare and characterize gentamicin (GM)-loaded poly(D,L-lactide-co-glycolide) (PLGA) microspheres.
- To investigate the factors influencing encapsulation efficiency (EE) and drug release behavior.
- To evaluate the potential of these microspheres as a sustained delivery system for gentamicin.
Main Methods:
- Microspheres were prepared using a double emulsion solvent evaporation technique.
- Characterization included assessment of microsphere shape, mean diameter, and encapsulation efficiency.
- Drug release profiles were determined over a 4-week period.
Main Results:
- Spherical microspheres with mean diameters ranging from 3 to 9 microm were obtained.
- Encapsulation efficiency varied significantly (3.4% to 90%), influenced by external aqueous phase volume and internal aqueous phase pH (optimal at pH 6).
- Higher nominal GM loading resulted in lower encapsulation efficiencies and faster drug release.
- A biphasic release pattern was observed, with an initial burst followed by sustained release for up to 4 weeks.
Conclusions:
- The double emulsion solvent evaporation method is effective for producing GM-loaded PLGA microspheres.
- Formulation parameters, including pH and loading concentration, significantly impact encapsulation efficiency and release kinetics.
- These PLGA microspheres demonstrate potential for sustained gentamicin delivery, with tunable release profiles.